Abstract
(−)-Norepinephrine is the predominant neurotransmitter of the sympathetic innervation of the heart. Racemic norepinephrine was labelled with carbon-11 and injected i.v. into Cynomolgus monkeys. Five minutes after injection there was a more than tenfold higher radioactivity in the heart than in adjacent tissue. Pretreatment with the norepinephrine reuptake inhibitor desipramine reduced the uptake by more than 80%. The high specific uptake of racemic [11C]norepinephrine indicates that enatiomerically pure (−)-[11C]norepinephrine has promising potential for detailed mapping of the sympathetic innervation of the human myocardium.
References
Axelrod J. The fate of adrenaline and noradrenaline. In: Vane J, Wolstenholme G, O'Connor M, eds.Adrenergic mechanisms. Boston: Little, Brown & Co; 1960:28–39.
Goldstein D, Brush J, Eisenhofer G, Stull R, Esler M. In vivo measurement of neuronal uptake of norepinephrine in the human heart.Circulation 1988;78:41–48.
Melon P, Schwaiger M. Imaging of metabolism and autonomic innervation of the heart by positron emission tomography.Eur J Nucl Med 1992;19:453–464.
Fowler J, MacGregor R, Ansari A, Atkins H, Wolf A. A new rapid synthesis of carbon-11 labeled norepinephrine hydrochloride.J Med Chem 1974;17:246–248.
Schwaiger M, Hutchins G, Wieland D. PET measurements of presynaptic sympathetic nerve terminals in the heart. In: Kuhl D, ed.In vivo imaging of neurotransmitter functions in brain, heart and tumors. Washington: American College of Nuclear Physicians; 1991:329–347.
Iversen L, Jarrot B, Simmonds M. Differences in the uptake, storage and metabolism of (+)- and (−)-noradrenaline.Br J Pharmacol 1971;43:845–855.
Garg B, Krell R, Sokolski T, Patil P. Steric aspects of adrenergic drugs XXII: retention of (+)- and (−)-norepinephrine by mouse heart.J Pharm Sci 1973;62:1126–1129.
Ding Y, Fowler J, Dewey S, et al. Comparison of high specific activity (−) and (+)-6-[18F]fluoronorepinephrine and 6-[18F]fluorodopamine in baboons: heart uptake, metabolism and the effect of desipramine.J Nucl Med 1993;34:619–629.
Någren K, Schoeps K, Halldin C, Swahn C, Farde L. Selective synthesis of racemic 1-11C-labelled norepinephrine, octopamine and phenylethanolamine using [11C]nitromethane.Appl Radiat Isot 1994;45 (in press).
Swahn C, Halldin C, Farde L. HPLC-method for determination of ligand metabolism during PET-studies.Ann Univ Turkuensis 1992;88:65–66.
Raismann R, Sette M, Pimoule C, Kanger S. High affinity3H-desipramine binding in the periphal and central nervous system: a specific site associated with the neuronal uptake of noradrenaline.Eur J Pharmacol 1982;78:345–351.
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Correspondence to: L. Farde
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Farde, L., Halldin, C., Någren, K. et al. Positron emission tomography shows high specific uptake of racemic carbon-11 labelled norepinephrine in the primate heart. Eur J Nucl Med 21, 345–347 (1994). https://doi.org/10.1007/BF00947971
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DOI: https://doi.org/10.1007/BF00947971